This invention relates to .gamma.-allenic-substituted amino acids and in particular, .gamma.-aminobutyric acid.
A number of studies have demonstrated that .gamma.-aminobutyric acid is a major inhibitory transmitter of the central nervous system (i.e. Y. Godin, et. al. Journal of Neurochemistry, 16, 869 (1969)). A perturbation of the excitation and inhibition interplay can lead to disease states such as Huntington's chorea, Parkinsonism, schizophrenia, epilepsy, depression, hyperkinesis and manic depressive disorders [Biochem. Pharmacol., 23, 2367-2649 (1974)]. A number of compounds, most notably .gamma.-monofluoromethyl-.gamma.-aminobutyric acid, .gamma.-acetylenic and .gamma.-vinyl-.gamma.-aminobutyric acid are potent irreversible inhibitors of .gamma.-aminobutyric acid transaminase and significantly increase the brain level of .gamma.-aminobutyric acid in animals rendering them useful in the treatment of the aforementioned disease states.
It has been found that .gamma.-allenyl-.gamma.-aminobutyric acid derivatives are potent inhibitors of .gamma.-aminobutyric acid transaminase.